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Identity And Pharmacological Mechanism — Quick Reference

By Editorial Desk · published 2026-05-03 · last reviewed 2026-05-21 · Info

A practical reference on Anti-doping testing: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

Reviewed 2026-05-21. Anything still debated is marked as such rather than presented as settled.

Identity and Pharmacological Mechanism

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Identity and Regulatory Status

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.

Cardarine at a glance

PropertyValueNotes
Chemical classSynthetic PPARδ agonistNot a steroid or a selective androgen receptor modulator.
Common synonymsCardarine, GW501516, GW-501516, endurobolNames vary by supplier and literature source.
AppearanceWhite to off-white powderConsistent with many small-molecule research chemicals.
SolubilityLow in water; soluble in DMSO and ethanolOften prepared in organic solvent for laboratory work.
Primary targetPPARδ (NR1C2)Nuclear receptor involved in lipid and energy metabolism.

Mechanism and Safety Research

Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.

GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.

Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.

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Detection, Stability, and Quality

Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.

Quality assessment for cardarine samples usually combines identity, purity, and impurity testing. Nuclear magnetic resonance spectroscopy and mass spectrometry can confirm molecular structure, while high-performance liquid chromatography estimates purity. Certificates of analysis from testing laboratories may list these results, but they do not establish safety or legality. In the absence of approved manufacturing, products sold online may contain the wrong compound, variable amounts, or unlisted contaminants. Independent verification is therefore central to analytical work and to interpreting any reported biological activity.

Laboratory detection of GW501516 commonly uses liquid chromatography coupled with tandem mass spectrometry. The method can identify the parent compound or its metabolites in urine and blood after sample cleanup. Protein precipitation, solid-phase extraction, or enzymatic hydrolysis may precede analysis, depending on the matrix. Reference standards are required for accurate quantification and confirmation. Because the compound is not approved, testing often occurs in anti-doping, forensic, or research settings rather than routine clinical care. Results are reported with limits of detection and quantification.

Detection and Regulatory Landscape

Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

Regulatory Status and Detection Context

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

Notes from published material

=== Dysplasia === Heart valve dysplasia is an error in the development of any of the heart valves, and a common cause of congenital heart defects in humans as well as animals; tetralogy of Fallot is a congenital heart defect with four abnormalities, one of which is stenosis of the pulmonary valve. Ebstein's anomaly is an abnormality of the tricuspid valve, and its presence can lead to tricuspid valve regurgitation. A bicuspid aortic valve is an aortic valve with only 2 cusps as opposed to the normal 3. It is present in about 0.5% to 2% of the general population and causes increased calcification due to higher turbulent flow through the valve.

== See also == Atomic absorption spectrophotometry Atomic emission spectroscopy Inductively coupled plasma atomic emission spectroscopy Inductively coupled plasma mass spectrometry LBOZ Microspectrophotometry Slope spectroscopy Spectroradiometry

== Detection == Separation by capillary electrophoresis can be detected by several detection devices. The majority of commercial systems use UV or UV-Vis absorbance as their primary mode of detection. In these systems, a section of the capillary itself is used as the detection cell. The use of on-tube detection enables detection of separated analytes with no loss of resolution. In general, capillaries used in capillary electrophoresis are coated with a polymer (frequently polyimide or Teflon) for increased flexibility. The portion of the capillary used for UV detection, however, must be optically transparent. For polyimide-coated capillaries, a segment of the coating is typically burned or scraped off to provide a bare window several millimeters long. This bare section of capillary can break easily, and capillaries with transparent coatings are available to increase the stability of the cell window. The path length of the detection cell in capillary electrophoresis (~ 50 micrometers) is far less than that of a traditional UV cell (~ 1 cm). According to the Beer-Lambert law, the sensitivity of the detector is proportional to the path length of the cell. To improve the sensitivity, the path length can be increased, though this results in a loss of resolution. The capillary tube itself can be expanded at the detection point, creating a "bubble cell" with a longer path length or additional tubing can be added at the detection point as shown in figure 2. Both of these methods, however, will decrease the resolution of the separation.

== Structure == PAR1 is a transmembrane G-protein-coupled receptor (GPCR) that shares much of its structure with the other protease-activated receptors. These characteristics include having seven transmembrane alpha helices, four extracellular loops and three intracellular loops. PAR1 specifically contains 425 amino acid residues arranged for optimal binding of thrombin at its extracellular N-terminus. The C-terminus of PAR1 is located on the intracellular side of the cell membrane as part of its cytoplasmic tail.

=== Atomic radius === Historically, the physical size of atoms was unknown until the early 20th century. The first calculated estimate of the atomic radius of hydrogen was published by physicist Arthur Haas in 1910 to within an order of magnitude (a factor of 10) of the accepted value, the Bohr radius (~0.529 Å). In his model, Haas used a single-electron configuration based on the classical atomic model proposed by J. J. Thomson in 1904, often called the plum-pudding model. Atomic radii (the size of atoms) are dependent on the sizes of their outermost orbitals. They generally decrease going left to right along the main-group elements, because the nuclear charge increases but the outer electrons are still in the same shell. However, going down a column, the radii generally increase, because the outermost electrons are in higher shells that are thus further away from the nucleus. The first row of each block is abnormally small, due to an effect called kainosymmetry or primogenic repulsion: the 1s, 2p, 3d, and 4f subshells have no inner analogues. For example, the 2p orbitals do not experience strong repulsion from the 1s and 2s orbitals, which have quite different angular charge distributions, and hence are not very large; but the 3p orbitals experience strong repulsion from the 2p orbitals, which have similar angular charge distributions. Thus higher s-, p-, d-, and f-subshells experience strong repulsion from their inner analogues, which have approximately the same angular distribution of charge, and must expand to avoid this.

Sources: en.wikipedia.org

Further detail

Recommendations are to include multiple types of exercise in exercise programs, and to prescribe exercise as early as possible in addition to medication, to gain the benefits of regular, long-term activity. Aerobic and resistance training exercise guidelines for Parkinson disease recommend 3–5 days per week of aerobic training (doing 20–60 minutes at moderate intensity) and 2–3 days per week of resistance training (doing 1-3 sets, of 8-12 repetitions, at between 40%-50% of the maximum for 1 repetition). Exercise is generally considered safe, with studies in PD reporting no serious adverse events and a very low risk of other events such as soreness, joint inflammation, fatigue, dizziness, or falls. Drop-out rates were comparable for exercising and non-exercising controls, with a generally high rate of exercise adherence.

A substance (other than food) intended to affect the structure or any function of the body. A substance intended for use as a component of a medicine but not a device or a component, part, or accessory of a device. A substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease. A substance recognized by an official pharmacopeia or formulary. Biological products are included within this definition and are generally covered by the same laws and regulations, but differences exist regarding their manufacturing processes (chemical process versus biological process).

=== Wild-type (ATTRwt-CM) === This type has no mutations in the TTR gene but TTR deposits still form in the heart and other tissues. Males are more commonly affected, at ages over 70 years. Carpal tunnel syndrome may form as well as amyloid deposits in the carpal tunnel causing compression of the median nerve. Amyloid deposits in the carpal tunnel or other ligaments (causing tendon rupture) or the spinal canal causing spinal stenosis may precede the development of heart failure by 10-15 years. Wild type ATTR cardiac amyloidosis (and the genetic variant) can be diagnosed with cardiac nuclear scintigraphy to visualize amyloid deposits in the heart walls. Serum free light chains, serum and urine electrophoresis with immunofixation can rule out AL amyloidosis. If the diagnosis is unclear, a biopsy may be obtained. Biopsy with histological evaluation can rule out light chain and genetic testing can rule out familial subtypes. This type is often misdiagnosed. However, greater use of cardiac magnetic resonance has increased the rate of diagnosis. The severity of the disease tends to be less than the light chain and familial variants. This is due to the amount of time that it takes to accumulate the amyloid depositions being longer in the wild-type variant.

Early grocery stores were "austere" and tiny by modern standards, with as few as 450 items. Shopping for groceries often involved trips to multiple specialty shops, such as a greengrocer, butcher, bakery, fishmonger and dry goods store, in addition to a general store. Milk and other items of short shelf life were delivered by a milkman. These small retailers were the final links in a "long and tortuous food chain," as most of them were far too small to deal directly with most of the persons who actually harvested, processed, and distributed all that food. During the 1920s, the highly inefficient nature of the American food distribution system meant that the "average urban family spent fully one-third of its budget on food". One of the most important defining features of the modern supermarket is cheap food. The vast abundance of cheap, wholesome food which modern consumers take for granted today was simply unimaginable before the middle of the 20th century, to the point that the first American supermarket customers in the 1930s were overcome with emotion at the sight of so much cheap food. Before the 20th century, food was neither cheap, nor wholesome, nor abundant. For example, in 1812, almost 90 percent of Americans worked in food production, and they struggled to stay alive on food which was often scarce, of poor quality, and riddled with diseases which could and did often kill them.

The third zone is called the Steady-State Zone (SSZ), macropores in this region are aligned with one another and grow in a regular fashion. Within the SSZ, the structure is defined by a value λ that is the average thickness of a ceramic wall and its adjacent macropore.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

How does cardarine interact with the body?

It binds to and activates PPARδ, a nuclear receptor that regulates genes related to fatty acid oxidation and energy use. This activation alters transcription in tissues such as skeletal muscle and liver. The full range of downstream effects in humans is not fully established.

Is cardarine found naturally?

No, cardarine is not known to occur naturally in plants, animals, or humans. It is a synthetic molecule produced for laboratory research. Products labeled as cardarine should therefore be treated as manufactured chemicals with variable purity.

Is cardarine a SARM?

No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.

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